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Your search keyword '"Karen L. Kage"' showing total 4 results
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4 results on '"Karen L. Kage"'

1. 767 Pre-clinical and first-in-human studies of HCW9218, a bifunctional TGF-β antagonist/IL-15 protein complex, in advanced solid tumors

Author

Peter R Rhode, Hing C Wong, Jack O Egan, Jeffrey S Miller, Manish Patel, Martin Felices, Philip M Arlen, Melissa A Geller, Pallavi Chaturvedi, Shannon Lunn, Bethany Hanke, Rose Wangen, Niraj Shrestha, Danieska Sandino, Karen L Kage, Delsy G Gaetano, Giles M Leclerc, Zhu Xiaoyun, Kelsey Mullen, and Deepa Kolaseri Krishnadas

Subjects
Neoplasms. Tumors. Oncology. Including cancer and carcinogens, RC254-282
Published
2023
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2. Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design

Author

Adrian D. Hobson, Russell A. Judge, Ana L. Aguirre, Brian S. Brown, Yifang Cui, Ping Ding, Eric Dominguez, Enrico DiGiammarino, David A. Egan, Gail M. Freiberg, Sujatha M. Gopalakrishnan, Christopher M. Harris, Marie P. Honore, Karen L. Kage, Nicolas J. Kapecki, Christopher Ling, Junli Ma, Helmut Mack, Mulugeta Mamo, Stefan Maurus, Bradford McRae, Nigel S. Moore, Bernhard K. Mueller, Reinhold Mueller, Marian T. Namovic, Kaushal Patel, Steve D. Pratt, C. Brent Putman, Kara L. Queeney, Kathy K. Sarris, Lisa M. Schaffter, Vincent Stoll, Anil Vasudevan, Lei Wang, Lu Wang, William Wirthl, and Kimberly Yach

Subjects
0301 basic medicine, rho-Associated Kinases, Cytochrome P-450 CYP2C9 Inhibitors, Drug Evaluation, Preclinical, Administration, Oral, Biological Availability, Crystallography, X-Ray, Mice, Inbred C57BL, Rats, Sprague-Dawley, Structure-Activity Relationship, 03 medical and health sciences, 030104 developmental biology, 0302 clinical medicine, Drug Design, Optic Nerve Injuries, 030220 oncology & carcinogenesis, Drug Discovery, Animals, Cytochrome P-450 CYP3A Inhibitors, Humans, Molecular Medicine, Protein Kinase Inhibitors, Half-Life
Abstract

A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor. Substitution (2-Cl, 2-NH

Published
2018
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3. Corrigendum: Design of Aminobenzothiazole Inhibitors of Rho Kinases 1 and 2 by Using Protein Kinase A as a Structure Surrogate

Author

Russell A. Judge, Anil Vasudevan, Victoria E. Scott, Gricelda H. Simler, Steve D. Pratt, Marian T. Namovic, C. Brent Putman, Ana Aguirre, Vincent S. Stoll, Mulugeta Mamo, Steven I. Swann, Steven C. Cassar, Connie R. Faltynek, Karen L. Kage, Janel M. Boyce-Rustay, and Adrian D. Hobson

Subjects
Organic Chemistry, Molecular Medicine, Molecular Biology, Biochemistry
Published
2018
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4. Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca²⁺ channel blockers with analgesic activity

Author

Xenia, Beebe, Daria, Darczak, Rodger F, Henry, Timothy, Vortherms, Richard, Janis, Marian, Namovic, Diana, Donnelly-Roberts, Karen L, Kage, Carol, Surowy, Ivan, Milicic, Wende, Niforatos, Andrew, Swensen, Kennan C, Marsh, Jill M, Wetter, Pamela, Franklin, Scott, Baker, Chengmin, Zhong, Gricelda, Simler, Erica, Gomez, Janel M, Boyce-Rustay, Chang Z, Zhu, Andrew O, Stewart, Michael F, Jarvis, and Victoria E, Scott

Subjects
Male, Rats, Sprague-Dawley, Analgesics, Disease Models, Animal, Structure-Activity Relationship, Calcium Channels, N-Type, Pyrrolidines, Behavior, Animal, Acetamides, Animals, Pain, Calcium Channel Blockers, Rats
Abstract

A novel 4-aminocyclopentapyrrolidine series of N-type Ca(2+) channel blockers have been discovered. Enantioselective synthesis of the 4-aminocyclopentapyrrolidines was enabled using N-tert-butyl sulfinamide chemistry. SAR studies demonstrate selectivity over L-type Ca(2+) channels. N-type Ca(2+) channel blockade was confirmed using electrophysiological recording techniques. Compound 25 is an N-type Ca(2+) channel blocker that produces antinociception in inflammatory and nociceptive pain models without exhibiting cardiovascular or motor liabilities.

Published
2012

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